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Sports Medicine

, Volume 7, Issue 2, pp 109–124 | Cite as

Opioids and Exercise

An Update
  • G. A. Sforzo
Research Review

Summary

A number of endogenously produced opioid peptides interact with centrally and peripherally located specific receptors to form a widespread neuroendocrine system with many implications for human function. It is becoming increasingly evident that moderately high and high intensity exercise stimulate the release of the opioid peptide β-endorphin to the circulation and this event may be subject to considerable intra- and interindividual variation. Moreover, endorphin levels probably remain elevated for 15 to 60 minutes following exercise. The duration of exertion does not seem to be critical, and low or moderate (< 75% V̇O2max) intensity efforts do not stimulate this response. It also appears (mostly from animal model research) that exercise might elicit central opioid effects, but there is conflicting evidence on this topic. Physical training may encourage adapted opioid system function (e.g. altered peptide response to exercise or receptor number), but these adaptations are not well elucidated by the few existing studies.

The significance of peripherally released opioid peptides during exercise has frequently been questioned. Exercise-induced affective response (e.g. mood enhancement), analgesia, food intake suppression and reproductive dysfunction are often mentioned as potentially controlled by an opioid mediated mechanism. While most of these events are normally considered under central control, it is time we begin entertaining the notion of peripheral effects (e.g. altered catecholamine release) and afferent input affecting central function in some of these phenomena. Additionally, evidence exists to suggest peripherally released enkephalins may cross the blood-brain barrier, but this is probably not true for endorphins. A number of other reported exercise-related events could possibly involve an underlying opioid mechanism. Exercise-associated metabolic regulation, immunosuppression, and cardiovascular function are areas for future opioid research.

Keywords

Naloxone Opioid Receptor Opioid Peptide Grade Exercise Test Endorphin Level 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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References

  1. Adams ML, Eastman NW, Tobin RP, Morris DL, Dewey WL. Increased plasma beta-endorphin immunoreactivity in scuba divers after submersion. Medicine and Science in Sports and Exercise 19: 87–90, 1987PubMedCrossRefGoogle Scholar
  2. Akil H, Young E, Walker JM, Watson SJ. The many possible roles of opioids and related peptides in stress-induced analgesia. Annals of the New York Academy of Sciences 467: 140–153, 1986PubMedCrossRefGoogle Scholar
  3. Banks WA, Kastin AJ. Saturable transport of peptides across the blood-brain barrier. Life Sciences 41: 1319–1338, 1987PubMedCrossRefGoogle Scholar
  4. Bjorntorp P. Effects of physical training on blood pressure in hypertension. European Heart Journal 8(Suppl. B): 71–76, 1987PubMedCrossRefGoogle Scholar
  5. Blake MJ, Stein EA, Vomachka AJ. Effects of exercise training on brain opioid peptides and serum LH in female rats. Peptides 5: 953–958, 1984PubMedCrossRefGoogle Scholar
  6. Blankstein J, Reyes FI, Winter JSD, Faimen C. Endorphins and the regulation of the human menstrual cycle. Clinical Endocrinology 14: 287–294, 1981PubMedCrossRefGoogle Scholar
  7. Blume AJ, Lichtshtein D, Boone G. Receptor-mediated inhibitions of NG108-15 adenylate cyclase: essential role of Na+ and GTP. In Pepeu et al. (Eds) Receptors for neurotransmitters and peptide hormones, pp. 339–348, Raven Press, 1980Google Scholar
  8. Bowen WD, Gentleman S, Herkenham M, Pert C. Interconverting mu and delta forms of the opiate receptor in rat striatal patches. Proceedings of the National Academy of Science 78: 4818–4822, 1981CrossRefGoogle Scholar
  9. Brambilla F, Facchinetti F, Petraglia F, Genazzani AR. Opioid peptides in primary affective disorders. In Muller & Genazzani (Eds) Central and peripheral endorphins, p. 265–277, Raven Press, New York, 1984Google Scholar
  10. Bramnert M, Hokfelt B. Lack of effect of naloxone in a moderate dosage on the exercise-induced increase in blood pressure, heart rate, plasma catecholamines, plasma renin activity and plasma aldosterone in healthy males. Clinical Science 68: 185–191, 1985PubMedGoogle Scholar
  11. Brooks S, Burrin J, Cheetham ME, Hall G, Williams C. The responses of the catecholamines and beta-endorphin to brief maximal exercise in man. European Journal of Applied Physiology and Occupational Physiology 57: 230–234, 1988PubMedCrossRefGoogle Scholar
  12. Bryant HU, Story JA, Yim GKW. Morphine-induced alterations in plasma and tissue cholesterol levels. Life Sciences 41: 545–554, 1987PubMedCrossRefGoogle Scholar
  13. Camilleci M, Malagelada R, Stanghellini V, Zinsmeister AR, Kao PC, et al. Dose-related effects of synthetic human beta-endorphin and naloxone on fed gastrointestinal motility. American Journal of Physiology 251: G147–G154, 1986Google Scholar
  14. Carr DB, Bullen BA, Skrinar GS, Arnold MA, Rosenblatt MA, et al. Physical conditioning facilitates the exercise induced secretion of beta-endorphin and beta-lipotropin in women. New England Journal of Medicine 305: 560–563, 1981PubMedCrossRefGoogle Scholar
  15. Colt EW, Wardlaw SL, Frantz AG. The effects of running on plasma beta-endorphin. Life Sciences 28: 1637–1640, 1981PubMedCrossRefGoogle Scholar
  16. Costa E, Mocchetti I, Supattapone S, Snyder S. Opioid peptide biosynthesis: enzymatic selectivity and regulatory mechanisms. FASEB Journal 1: 16–21, 1987PubMedGoogle Scholar
  17. Coupar I. Opioid action on the intestine: the importance of the intestinal mucosa. Life Sciences 41: 917–925, 1987PubMedCrossRefGoogle Scholar
  18. Cumming DC, Wheeler GD. Opioids in exercise physiology. Seminars in Reproductive Endocrinology 5: 171–179, 1987CrossRefGoogle Scholar
  19. Dearman J, Francis KT. Plasma levels of catecholamine, cortisol, and beta-endorphin in male athletes after running 26.2, 6 and 2 miles. Journal of Sports Medicine 23: 30–38, 1983Google Scholar
  20. deMeirleir K, Naaktgeboren N, VanSteirteghen A, Gorus F, Olbrecht J, et al. Beta-endorphin and ACTH levels in peripheral blood during and after aerobic and anerobic exercise. European Journal of Applied Physiology 55: 5–8, 1986CrossRefGoogle Scholar
  21. Donevan RH, Andrew GM. Plasma beta-endorphin immunoreactivity during graded cycle ergometry. Medicine and Science in Sports and Exercise 19: 229–233, 1987PubMedCrossRefGoogle Scholar
  22. Farrell PA, Gustafson AB, Morgan WP, Pert CB. Enkephalins, catecholamines, and psychological mood alterations: effects of prolonged exercise. Medicine and Science in Sports and Exercise 19: 347–353, 1987aPubMedCrossRefGoogle Scholar
  23. Farrell PA, Kjaer M, Bach FW, Galbo H. Beta-endorphin and adrenocorticotropin response to supramaximal treadmill exercise in trained and untrained males. Acta Physiologica Scandinavica 130: 619–625, 1987bPubMedCrossRefGoogle Scholar
  24. Feldberg W, Shaligram SV. The hyperglycaemic effect of morphine. British Journal of Pharmacology 46: 602–618, 1972PubMedCrossRefGoogle Scholar
  25. Feldman M, Kiser RS, Unger RH, Li CH. Beta-endorphin and the endocrine pancreas: studies in healthy and diabetic human beings. New England Journal of Medicine 308: 349–353, 1983PubMedCrossRefGoogle Scholar
  26. Feuerstein G, Siren A. Cardiovascular effects of enkephalins. Atlas of Science: Pharmacology 1: 280–283, 1987Google Scholar
  27. Fridland GH, Desiderio DM. Measurement of opioid peptides with combinations of reversed phase high performance liquid chromatography, radioimmunoassay, radioreceptorassay, and mass spectometry. Life Sciences 41: 809–812, 1987PubMedCrossRefGoogle Scholar
  28. Geller EB, Rowan CH, Adler MW. Body temperature effects of opioids in rats: intracerebroventricular administration. Pharmacology, Biochemistry and Behavior 24: 1761–1765, 1986CrossRefGoogle Scholar
  29. Gero A. Considerations on the nature of mu, kappa, and delta receptors. National Institute Drug Abuse Research Monogram Series 75: 37–40, 1986Google Scholar
  30. Gillman MA, Katzeff IE. Does opioid uncoupling of adrenal responses mediate opioid anti-stress effects? Medical and Science Research 16: 207–209, 1988Google Scholar
  31. Giugliano D, Cozzolino D, Salvatore T, Ceriello A, Torella R. Dual effect of beta-endorphin on insulin secretion in man. Hormonal and Metabolic Research 19: 502–503, 1987CrossRefGoogle Scholar
  32. Giugliano D, Torella R, Lefebvre PJ, Onofrio FD. Opioid peptides and metabolic regulation. Diabetalogia 31: 3–15, 1988Google Scholar
  33. Goldfarb AH, Hatfield BD, Sforzo GA, Flynn MG. Serum beta-endorphin levels during a graded exercise test to exhaustion. Medicine and Science in Sports and Exercise 19: 78–82, 1987PubMedCrossRefGoogle Scholar
  34. Gullestad L, Oystein Dolva L, Kjeldsen SE, Eide I, Kjekshus J. The effects of naloxone and timolol on plasma catecholamine levels during short term dynamic exercise. Scandinavian Journal of Clinical and Laboratory Investigation 47: 847–851, 1987PubMedCrossRefGoogle Scholar
  35. Harber VJ, Sutton JR. Endorphins and exercise. Sports Medicine 1: 154–171, 1984PubMedCrossRefGoogle Scholar
  36. Hawkins KN, Knapp RJ, Gehlert DR, Lui GK, Yamamura MS, et al. Quantitative autoradiography of [3H]CTOP binding to mu opioid receptors in the rat brain. Life Sciences 42: 2541–2551, 1988PubMedCrossRefGoogle Scholar
  37. Herz A. Multiple endorphins as natural ligands for multiple opioid receptors. In Muller & Genazzani (Eds) Central and peripheral endorphins, pp. 43–52, Raven Press, New York, 1984Google Scholar
  38. Holaday JW, Tortella FC. Multiple opioid receptors: possible physiological functions of mu and delta binding sites in vivo. In Muller & Genazzani (Eds) Central and peripheral endorphins, pp. 237–250, Raven Press, New York, 1984Google Scholar
  39. Houghten RA, Pratt SM, Young EA, Brown H, Spann DR. Effect of chronic exercise on beta-endorphin receptor levels in rats. National Institute Drug Abuse Research Monogram Series 75: 505–508, 1986Google Scholar
  40. Howlett T, Tomlin S, Ngahfoong L, Bullen BA, Skrinar GS, et al. Exercise-induced release of met-enkephalin and beta-endorphin. In Muller & Genazzani (Eds) Central and peripheral endorphins, pp. 285–288, Raven Press, New York, 1984Google Scholar
  41. Hughes J. Biogenesis, release and inactivation of enkephalins and dynorphins. British Medical Bulletin 39: 17–24, 1983PubMedGoogle Scholar
  42. Hughes J, Kosterlitz HW. Introduction. British Medical Bulletin 39: 1–3, 1983PubMedGoogle Scholar
  43. Inosotroza J, Teschemacher HJ, Mueller-Eckhardt C. Opioid peptides and the immune system. Immunologia 6: 93–99, 1987Google Scholar
  44. Johnson HM, Smith EM, Torres BA, Blalock JE. Regulation of the in vitro antibody response by neuroendocrine hormones, Proceedings of the National Academy of Science 79: 4171–4174, 1982CrossRefGoogle Scholar
  45. Kastin AJ, Olson GA, Zadina JE, Olson RD. Disparate effects of peripherally administered endorphins and enkephalins in laboratory animals. In Muller & Genazzani (Eds) Central and peripheral endorphins, pp. 99–108, Raven Press, New York, 1984Google Scholar
  46. Keast D, Cameron K, Morton AR. Exercise and the immune response. Sports Medicine 5: 248–267, 1988PubMedCrossRefGoogle Scholar
  47. Langenfeld ME, Hart LS, Kao PC. Plasma beta-endorphin responses to one-hour bicycling and running at 60% V̇D2max. Medicine and Science in Sports and Exercise 19: 83–86, 1987PubMedCrossRefGoogle Scholar
  48. Levine JD, Gordon NW, Fields NL. Naloxone dose-dependently produces analgesia and hyperalgesia in postoperative patients. Nature 278: 740, 1979PubMedCrossRefGoogle Scholar
  49. Lolait SJ, Lim ATW, Toh BH, Funder JW. Immunoreactive β-endorphin in a subpopulation of mouse spleen macrophages. Journal of Clinical Investigation 73: 277–280, 1984PubMedCrossRefGoogle Scholar
  50. Madison DV, Nicoll RA. Enkephalin hyperpolarizes interneurons in the rat hippocampus. Journal of Physiology 398: 123–130, 1988PubMedGoogle Scholar
  51. Martinez JL, Weinberger SB, Scholteis G. Enkephalins and learning and memory: a review of evidence for a site of action outside of the blood-brain barrier. Behavioral and Neural Biology 49: 192–221, 1988PubMedCrossRefGoogle Scholar
  52. Matthews PM, Froelich CJ, Sibbitt WL, Bankhurst AD. Enhancement of natural cytotoxicity by beta-endorphin. Journal of Immunology 130: 1658–1662, 1983Google Scholar
  53. McCain HW, Lamster IB, Bilotta J. Modulation of human T-cell suppressor activity by beta-endorphin and glycyl-1-glutamine. International Journal of Immunopharmacology 8:443–446,1986PubMedCrossRefGoogle Scholar
  54. McMurray RG, Forsythe WA, Mar MH, Hardy CJ. Exercise intensity-related responses of beta-endorphin and catecholamines. Medicine and Science in Sports and Exercise 19: 570–574, 1987PubMedCrossRefGoogle Scholar
  55. Metzger JM, Stein EA. Brain endorphin and sprint training. Life Sciences 34: 1541–1547, 1984PubMedCrossRefGoogle Scholar
  56. Miller BE, Lipman JJ, Byrne WL. Partial characterization of a novel endogenous opioid in human cerebrospinal fluid. Life Sciences 41: 2535–2545, 1987PubMedCrossRefGoogle Scholar
  57. Morley JE, Kay NE, Solomon GF, Plotnikoff NP. Neuropeptides: conductors of the immune orchestra. Life Sciences 41: 527–544, 1987PubMedCrossRefGoogle Scholar
  58. Mougin C, Baulay A, Henriet MT, Haton D, Jacquier MC, et al. Assessment of plasma opioid peptides, beta-endorphin and metenkephalin, at the end of an international ski race. European Journal of Applied Physiology 56: 281–286, 1987CrossRefGoogle Scholar
  59. Moss IR, Scarpelli EM. Beta-endorphin central depression of respiration and circulation. Journal of Applied Physiology 50: 1011–1016, 1981PubMedGoogle Scholar
  60. Olson GA, Olson R, Kastin AJ. Endogenous opioids: 1986. Peptides 8: 1135–1164, 1987PubMedCrossRefGoogle Scholar
  61. Oltras CM, Mora F, Vives F. Beta-endorphin and ACTH in plasma: effects of physical and psychological stress. Life Sciences 40: 1683–1686, 1987PubMedCrossRefGoogle Scholar
  62. Pasternak GW, Wood PJ. Multiple mu opioid receptors. Life Sciences 38: 1889–1898, 1986PubMedCrossRefGoogle Scholar
  63. Patterson SJ, Robson LE, Kosterlitz HW. Classification of opioid receptors. British Medical Journal 39: 31–36, 1983Google Scholar
  64. Pomeroy G, Ardell JL, Wurster RD. Spinal opioid modulation of cardiovascular reflexes in the exercising dog. Brain Research 381: 385–389, 1986PubMedCrossRefGoogle Scholar
  65. Rahkila P, Hakala E, Alen M, Salminen K, Laatikainen T. Beta-endorphin and corticotropin release is dependent on a threshold intensity of running in male endurance athletes. Life Sciences 43: 551–558, 1988PubMedCrossRefGoogle Scholar
  66. Rahkila P, Hakala E, Salminen K, Laatikainen T. Responses of plasma endorphins to running exercises in male and female endurance athletes. Medicine and Science in Sports and Exercise 19: 451–455, 1987PubMedCrossRefGoogle Scholar
  67. Rauramo I, Salminen K, Laatikainen T. Release of beta-endorphin in response to physical exercise in non-pregnant and pregnant women.Acta Obstetrica et Gynaecologica Scandinavica65: 609–612, 1986CrossRefGoogle Scholar
  68. Richter WO, Kerscher P, Janetschek P, Schwandt P. In vitro lipolysis of proopiocortin peptides. Life Sciences 33(Suppl. 1): 747–750, 1983PubMedCrossRefGoogle Scholar
  69. Richter WO, Kerscher P, Schwandt P. Beta-endorphin stimulates in vivo lipolysis in the rabbit. Life Sciences 33(Suppl. 1): 743–746, 1983PubMedCrossRefGoogle Scholar
  70. Richter WO, Schwandt P. Metabolic effects of beta-lipotropin in vivo and in vitro in the rabbit. In Muller & Genazzani (Eds) Central and peripheral endorphins, pp. 197–201, Raven Press, New York, 1984Google Scholar
  71. Schwellnus MP, Gordon NF. Effect of opioid antagonism on esophageal temperature during exercise. Medicine and Science in Sports and Exercise 20: 381–384, 1988PubMedCrossRefGoogle Scholar
  72. Seeger TF, Sforzo GA, Pert CB, Pert A. In vivo autoradiography: visualization of stress-induced changes in opiate receptor occupancy in the rat brain. Brain Research 305: 303–311, 1984PubMedCrossRefGoogle Scholar
  73. Sforzo GA. Opioids and exercise: a review. In Nudel (Ed.) Pediatric sports medicine, Ch. 4, SP Medical and Scientific, New York, 1988Google Scholar
  74. Sforzo GA, Seeger TF, Pert CB, Pert A, Dotson CO. In vivo opioid receptor occupation in the rat brain following exercise. Medicine and Science in Sports and Exercise 18: 380–384, 1986PubMedCrossRefGoogle Scholar
  75. Sheps DS, Koch G, Bragdon EE, Ballenger MN, McMurray RG. The reproducibility of resting and post-exercise plasma beta-endorphins. Life Sciences 43: 787–791, 1988PubMedCrossRefGoogle Scholar
  76. Shippenberg TS, Herz A. Differential effects of mu and kappa opioid systems on motivational processes. National Institute Drug Abuse Research Monogram Series 75: 563–566, 1986Google Scholar
  77. Smyth DG. Beta-endorphin and related peptides in pituitary, brain, pancreas and antrum. British Medical Journal 39: 25–30, 1983Google Scholar
  78. Solerte SB, Fiorauanti M, Petraglia F, Facchinetti F, Patti AL, et al. Plasma beta-endorphin, free fatty acid and blood lipid changes in type 2 (non-insulin dependent) diabetic patients. Journal of Endocrinological Investigation 11: 37–42, 1988PubMedGoogle Scholar
  79. Sonka K, Sonka J. Exercise and beta-endorphin in plasma. In Macek & Kucera (Eds) Sports in health and disease, pp. 150–152, Czechoslovak Medical Press, Prague, 1985Google Scholar
  80. Staessen J, Fiocchi R, Bouillon R, Fagard R, Lijnen P. The nature of opioid involvement in the hemodynamic respiratory and humoral responses to exercise. Circulation 72: 982–990, 1985PubMedCrossRefGoogle Scholar
  81. Staessen J, Fiocchi R, Fagard R, Lijnen P, Amery A. Alpha-adrenoceptor blockade by tibalosine: hemodynamic and humoral effects at rest and during exercise, and effect of opioid receptor antagonism. Journal of Cardiovascular Pharmacology 8: 1028–1034, 1986PubMedCrossRefGoogle Scholar
  82. Terenius L, Nyberg F. Opioid peptides in man–analytical aspects. Life Sciences 41: 805–808, 1987PubMedCrossRefGoogle Scholar
  83. Vettor R, Manno M, DeCarlo E, Federspil G. Evidence for an involvement of opioid peptides in exercise-induced lipolysis in rats. Hormonal and Metabolic Research 19: 282–283, 1987CrossRefGoogle Scholar
  84. Viswanathan M, VanDijk JP, Graham TE, Bonen A, George JC. Exercise and cold-induced changes in plasma beta-endorphin and beta-lipotropin in men and women. Journal of Applied Physiology 62: 622–627, 1987PubMedGoogle Scholar
  85. Wagner HN. Quantitative imaging of dopamine, serotonin, and opiate receptors in the living human brain. In Boast et al. (Eds) Quantitative receptor autoradiography, pp. 233–254, Liss Inc., Philadelphia, 1986Google Scholar
  86. Wardlaw SL, Frantz A. Effects of swimming stress on brain beta-endorphin and ACTH. Clinical Research 28: 482A, 1980Google Scholar
  87. Weber RJ, Pert CB. Opiatergic modulation of the immune system. In Muller & Genazzani (Eds) Central and peripheral endorphins, pp. 35–42, Raven Press, New York, 1984Google Scholar
  88. Zagon IS, McLaughlin PJ. Naltrexone’s influence on neurobehavioral development. Pharmacology, Biochemistry and Behavior 22: 441–448, 1985CrossRefGoogle Scholar

Copyright information

© ADIS Press Limited 1989

Authors and Affiliations

  • G. A. Sforzo
    • 1
  1. 1.School of Health Sciences and Human PerformanceIthaca CollegeIthacaUSA

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